Synthesis and Bioactivity of New Chalcone Derivatives as Potential Tyrosinase Activator Based on the Click Chemistry |
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| Authors: | Chao Niu Gen Li Adila Tuerxuntayi Haji A Aisa |
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| Institution: | 1. Key Laboratory of Plant Resources and Chemistry of Arid Zone, Chinese Academy of Sciences, Urumqi, Xinjiang 830011, China;2. State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, Xinjiang 830011, China |
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| Abstract: | A new series of (E)‐1‐(4‐((1‐benzyl‐1H‐1,2,3‐triazol‐4‐yl)methoxy)phenyl)‐3‐phenylprop‐2‐en‐1‐one 1a (4‐((1‐benzyl‐1H‐1,2,3‐triazol‐4‐yl) methoxy)phenyl)‐1‐phenylprop‐2‐en‐1‐one 1b – 15b were designed, synthesized based on click chemistry, and biologically evaluated for their activity on tyrosinase. The result showed that most of prepared compounds 1a – 15a have potent activating effect on tyrosinase, especially for 3a , 8a – 10a and 14a – 15a . Among them, compounds 10a and 14a demonstrated the best activity with EC50=1.71 and 5.60 µmol·L?1 respectively, even better than the positive control 8‐MOP (EC50=14.8 µmol·L?1). Conversely, compounds 3b , 5b – 6b , 9b – 10b , and 15b induced enzymatic inhibition on tyrosinase. |
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| Keywords: | enzyme chalcone heterocycles synthesis structure‐activity relationship |
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